Method for detecting compounds modulating dimers of vft domain membrane proteins

a technology of vft domain and dimer, which is applied in the field of compound modulating membrane receptors, can solve the problems of inability to use screening methods on a large scale, poor suitability of existing techniques for demonstrating compounds capable of modulating the activation of dimeric class c gpcrs, and difficult detection of agonist effects
US20120115176A1Active Publication Date: 2012-05-10CIS BIO INT +1
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Patent Information

Authority / Receiving Office
US · United States
Current Assignee / Owner
CIS BIO INT
Publication Date
2012-05-10

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Abstract

The invention relates to a method for selecting compounds having a modulating effect on the activation state of a dimer of VFT-domain proteins expressed in cell membranes present in a measuring medium, said dimer consisting of a first protein and of a second protein, said proteins being identical or different, wherein this method comprises the following steps:(a) labeling the first and second proteins in the N-terminal portion of their VFT domains with the members of a pair of FRET partners, the Förster radius (R0) of said pair being between 20 and 55 Å;(b) measuring the FRET signal in the absence and in the presence of the test compound within a predetermined time window;(c) selecting the test compound as a modulating compound if a difference in FRET signal in the absence and in the presence of test compound is measured in step (b).The invention can be used in the search for new medicaments and new taste modulators.
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Description

PRIOR ART

[0001] The invention relates to compounds modulating membrane receptors which are of interest in the search for new medicaments and for new taste modulators and in agriculture.

[0002] G-protein coupled receptors (GPCRs) constitute the largest family of mammalian membrane receptors since they represent 3.4% of the genome. The isolation and then the cloning of GPCRs have made it possible to identify, in humans, around 900 genes, of which approximately 500 correspond to olfactory and taste receptors and 400 to receptors capable of binding endogenous ligands. Thus, the heterogeneity of these receptors provides a very broad recognition of both external signals (odors, light, taste molecules) and internal signals (hormones and neurotransmitters).

[0003] GPCRs are referenced in three major classes:

[0004] Class A, with rhodopsin being the archetype, is the most widely represented class. The binding site for the ligands of these receptors involves mainly the transmembrane domains and also...

Claims

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